1210045-17-2Relevant academic research and scientific papers
IMIDAMIDE SPHINGOSINE KINASE INHIBITORS
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Page/Page column 24, (2012/09/05)
Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 and SphK2) are provided. The compounds can prevent angiogenesis in tumors.
Discovery, biological evaluation, and structure-activity relationship of amidine based sphingosine kinase inhibitors
Mathews, Thomas P.,Kennedy, Andrew J.,Kharel, Yugesh,Kennedy, Perry C.,Nicoara, Oana,Sunkara, Manjula,Morris, Andrew J.,Wamhoff, Brian R.,Lynch, Kevin R.,MacDonald, Timothy L.
experimental part, p. 2766 - 2778 (2010/09/04)
Sphingosine 1-phosphate (S1P), a potent phospholipid growth and trophic factor, is synthesized in vivo by two sphingosine kinases. Thus these kinases have been proposed as important drug targets for treatment of hyperproliferative diseases and inflammation. We report here a new class of amidine-based sphingosine analogues that are competitive inhibitors of sphingosine kinases exhibiting varying degrees of enzyme selectivity. These inhibitors display KI values in the submicromolar range for both sphingosine kinases and, in cultured vascular smooth muscle cells, decrease S1P levels and initiate growth arrest.
